Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics

Bioorganic & Medicinal Chemistry Letters
2004.0

Abstract

A new series of antibacterial ketolides is reported, which features the use of a C-6 carbamate for tethering the arylalkyl sidechain to the macrolide core. The best members of this series display in vitro and in vivo activity comparable to telithromycin. Partial epimerization at C-2, unobserved in previously reported ketolides, was noted for this series.

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